期刊
BRITISH JOURNAL OF CANCER
卷 114, 期 5, 页码 519-523出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/bjc.2016.20
关键词
Multiple Myeloma; HIF-1 alpha; p300; Chetomin; Targeted therapy
类别
资金
- French INCA (Institut National du Cancer) Institute [2012-109/087437]
- Languedoc Roussillon CRLR [R14026FF]
- Fondation de France [201400047510]
- ITMO Cancer (MMTT)
- AXLR SATT [30041633]
- Guillaume Espoir association (Saint-Genis-Laval, France)
Background: Multiple myeloma (MM) is an incurable clonal plasma cell malignancy. The constitutive expression of HIF-1 alpha in MM suggests that inhibition of HIF-1a-mediated transcription represents an interesting target in MM. Methods: As p300 is a crucial co-activator of hypoxia-inducible transcription, disrupting the complex HIF-1 alpha/p300 to target HIF activity appears to be an attractive strategy. Results: We reported that chetomin, an inhibitor of HIF-1 alpha/p300 interaction, exhibits antitumour activity in human myeloma cell lines and primary MM cells from patients. Conclusions: Our data suggest that chetomin may be of clinical value in MM and especially for patients characterised by a high EP300/HIF-1 alpha expression and a poor prognosis.
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